Synthesis and Biological Evaluation of 6-Substituted Mangiferin Derivatives as Antioxidant and Anticancer agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Mohan H. Patil ◽  
Uma D. Kabra ◽  
Krishna R. Gupta ◽  
Milind J. Umekar
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Anticancer Activities ◽  
Standard Drug ◽  
Chemical Structures ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of ◽  
Better Than

: Esterified and alkyl amine derivatives of mangiferin were synthesized and evaluated for in vitro antioxidant and anticancer activities. The chemical structures of the derivatives were confirmed using elemental analysis and spectral data.The antioxidant activity was assessed using 2,2-diphenyl-1-picrylhydrazy (DPHH) assay and some derivatives displayed antioxidant activity better than mangiferin and standard drug ascorbic acid. Among the synthesized derivatives, few exhibited enhanced anticancer activity against human breast (MDA-MB-231) cancer cell lines, then the parent mangiferin.

Construction of C-glycosides of heterocycles containing the pyrimidin-2-amine or the 1H-pyrazolo[3,4-b]pyridine moiety and their biological evaluation for anticancer activities

2019 ◽  
Vol 43 (3-4) ◽  
pp. 152-157
Author(s):  
Wu-Wu Li ◽  
Min-Yan Zheng ◽  
Ying Guo ◽  
Zun-Ting Zhang ◽  
Ji-Chang Han ◽  
...  
Keyword(s):  
High Resolution Mass Spectrometry ◽  
Positive Control ◽  
Biological Evaluation ◽  
Human Leukemia ◽  
Anticancer Activities ◽  
Standard Drug ◽  
Chemical Structures ◽  
Pyridine Moiety ◽  
Heterocyclic Derivatives

A series of novel C-glycosides of heterocyclic derivatives containing a pyrimidin-2-amine or a 1 H-pyrazolo[3,4- b]pyridine moiety were synthesized using condensation reactions of the substituted puerarin with guanidine or 3-amino-5-hydroxypyrazole in methyl alcohol. Their chemical structures were characterized by Fourier-transform infrared spectroscopy, nuclear magnetic resonance, and high-resolution mass spectrometry. In addition, their biological activity has been demonstrated by in vitro evaluation against the human leukemia cells K562 and human prostate cancer cells PC-3 by MTT-based assays, using the commercially available standard drug of cis-platin as a positive control. The results also demonstrated that most of the compounds showed considerable cytotoxicity to these two cell lines of K562 and PC-3, and indicated that novel C-glycosides of heterocyclic derivatives may be potential leads for further biological screenings and may generate drug-like molecules.

Synthesis and biological evaluation of novel fluorinated anticancer agents incorporating the indolin-2-one moiety

RSC Advances ◽  
2015 ◽  
Vol 5 (111) ◽  
pp. 91795-91801 ◽  
Author(s):  
Shuai-Yu Wang ◽  
Li-Jun Wang ◽  
Bo Jiang ◽  
Ning Wu ◽  
Xiang-Qian Li ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Anticancer Activities ◽  
Synthesis And Biological Evaluation

A series of novel fluorinated anticancer agents containing the indolin-2-one moiety were designed, synthesized and evaluated for their anticancer activities in vitro.

Synthesis and biological evaluation of novel derivatives of gambogenic acid as anticancer agents

MedChemComm ◽  
2015 ◽  
Vol 6 (2) ◽  
pp. 334-338 ◽  
Author(s):  
Peng Huang ◽  
Zhong Hu ◽  
Liqin He ◽  
Xiaoshan Wang ◽  
Yaxian Wu
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Antiproliferative Activity ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel derivatives of gambogenic acid (GNA) were synthesized and evaluated for their in vitro antiproliferative activity against four kinds of tumor cell lines. These compounds displayed potent antiproliferative activity. In particular, compound 3f exhibited superior antiproliferative activity against these tumor cell lines than GNA.

Design, synthesis and biological evaluation of rhein derivatives as anticancer agents

MedChemComm ◽  
2016 ◽  
Vol 7 (9) ◽  
pp. 1812-1818 ◽  
Author(s):  
Junkai Huang ◽  
Zhuo Zhang ◽  
Peng Huang ◽  
Liqin He ◽  
Yong Ling
Keyword(s):  
Tumor Cell ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Promising Candidate ◽  
Design Synthesis ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel derivatives of rhein were synthesized and evaluated for their in vitro antiproliferative activity against six kinds of tumor cell lines. All derivatives displayed more potent anti-tumor activity than rhein, and most of them were even stronger than 5-FU. Compound 4v was the most promising candidate among the investigated compounds.

Hybridized Quinoline Derivatives as Anticancer Agents: Design, Synthesis, Biological Evaluation and Molecular Docking

2019 ◽  
Vol 19 (4) ◽  
pp. 439-452 ◽  
Author(s):  
Mohamed R. Selim ◽  
Medhat A. Zahran ◽  
Amany Belal ◽  
Moustafa S. Abusaif ◽  
Said A. Shedid ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Caspase 3 ◽  
Biological Evaluation ◽  
Tubulin Polymerization ◽  
Design Synthesis ◽  
Chemical Structures ◽  
M Phase ◽  
Induced Apoptosis ◽  
Derivatives Of

Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]

2017 ◽  
Vol 46 (21) ◽  
pp. 7005-7019 ◽  
Author(s):  
Benjamin W. J. Harper ◽  
Emanuele Petruzzella ◽  
Roman Sirota ◽  
Fernanda Fabiola Faccioli ◽  
Janice R. Aldrich-Wright ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Synthesis and biological evaluation in vitro and in vivo of functionalized Pt(iv) derivatives of Pt56MeSS.

scholarly journals Synthesis and biological evaluation of 4-substituted aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione as anti-cancer and anti-angiogenesis agents

2020 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Chemical Structures ◽  
Piperazine Derivatives ◽  
Anti Cancer ◽  
Ic50 Values ◽  
And Migration ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC50＞79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC50=65.3μM), it indeed significantly abrogated endothelia cell migration (IC50=6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.

scholarly journals Synthesis and biological evaluation of 4-substituted aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione as anti-cancer and anti-angiogenesis agents

2020 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
H Nmr ◽  
Chemical Structures ◽  
Piperazine Derivatives ◽  
Anti Cancer ◽  
And Migration ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.0 2,6 ] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1 H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC 50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC 50 ＞ 79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC 50 =65.3μM), it indeed significantly abrogated endothelia cell migration (IC 50 =6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.

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